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Table 1 Study 1: Pharmacokinetic parameters of riociguat in plasma after a single oral dose of riociguat (pharmacokinetic analysis population, n=29):

From: Bioavailability, pharmacokinetics and safety of riociguat given as an oral suspension or crushed tablet with and without food

Parameter

Unit

n

2.4 mg high-concentration suspension fasted

n

2.4 mg high-concentration suspension fed

n

0.3 mg high-concentration suspension fasted

n

0.15 mg low-concentration suspension fasted

n

mgIR tablet fasted

AUC

μ*h/L

29

781/49 (230–1515)

29

663/45 (258–1212)

27

91/43 (38–165)

25

47/60 (8.3–91)

29

311/46 (103–587)

AUC/D

h/L

29

0.33/49 (0.10–0.63)

29

0.28/45 (0.12–0.50)

27

0.30/43 (0.13–0.55)

25

0.31/60 (0.056–0.61)

29

0.31/46 (0.10–0.59)

Cmax

μ/L

29

78/31 (43–128)

29

48/22 (32–70)

29

9.8/33 (4.5–17)

29

4.9/35 (1.9–8.1)

29

36/30 (18–61)

Cmax/D

1/L

29

0.03/31 (0.02–0.05)

29

0.02/22 (0.01–0.29)

29

0.03/33 (0.01–0.06)

29

0.03/35 (0.01–0.05)

29

0.04/30 (0.02–0.06)

tmaxa

h

29

1.5 (0.75–4.0)

29

4.0 (3.0–12)

29

1.0 (0.50–3.0)

29

1.0 (0.50–4.0)

29

1.0 (0.50–3.0)

t1/2

h

29

9.2/41 (2.8–21)

29

9.4/33 (4.2–17)

27

7.8/39 (3.5–15)

25

6.8/42 (2.5–12)

29

7.9/43 (3.4–14)

  1. Data presented as geometric mean/% coefficient of variation (range) unless otherwise specified.
  2. a Median (range)
  3. AUC, area under the concentration versus time curve; AUC/D; AUC divided by dose; Cmax, maximum drug concentration in plasma; Cmax/D: Cmax divided by dose; IR, immediate-release; tmax; time to reach Cmax; t1/2; half life